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AG14361 Chemical Structure

AG14361

Data Sheet For research use only. Not for human use.
Cat. No. :BCP02449CAS No. :328543-09-5Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 328543-09-5 Cat. No. BCP02449
Name AG14361
Synonyms AG-14361;AG 14361;
SMILES
Chemical Name
Formula C19H20N4O M. Wt 320.39
Purity 98% Storage Store at 4-8°C
Description AG14361 is at least 1000-fold more potent than the benzamides. The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells. Crystallographic analysis of AG14361 bound to the catalytic domain of chicken PARP-1 shows that the tricyclic ring system of AG14361 is located in a pocket composed of amino acid residues Trp861, His862, Gly863, Tyr896, Phe897, Ala898, Lys903, Ser904, Tyr907, and Glu988. AG14361 forms important hydrogen bonds with Ser904 and Gly863 and a water-mediated hydrogen bond with Glu988. AG14361-induced growth inhibition is not attributed to PARP-1-related effects because maximal PARP-1 inhibition is observed at much lower concentrations (≤1 μM) than the GI50. AG14361 at 0.4 μM does not affect cancer cell gene expression or growth, but it increases the antiproliferative activity of temozolomide and topotecan, and inhibits recovery from potentially lethal γ-radiation damage in LoVo cells by 73%. In addition, 0.4 μM AG14361 does not substantial
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